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Publication

Microwave-assisted synthesis of C-8 aryl and heteroaryl inosines and determination of their inhibitory activities against Plasmodium falciparum purine nucleoside phosphorylase

Journal Contribution - Journal Article

8-Arylinosines have been scarcely studied for therapeutic purposes, probably due to difficulties in their synthesis. The recently described direct arylation reaction at position 8 of purine nucleosides has been employed to synthesize a series of 8-aryl and 8-pyridylinosines. These compounds have been studied for hydrolytic stability and subjected to biological evaluation. Three compounds have shown a pronounced specific inhibition of Plasmodium falciparum-encoded purine nucleoside phosphorylase, an important target for antimalarial chemotherapy.
Journal: European Journal of Medicinal Chemistry
ISSN: 0223-5234
Volume: 82
Pages: 459 - 465
Publication year:2014
BOF-keylabel:yes
IOF-keylabel:yes
BOF-publication weight:3
CSS-citation score:1
Authors:International
Authors from:Higher Education
Accessibility:Closed